HRP20160168T1 - Crystalline forms of a macrolide, and uses therefor - Google Patents

Crystalline forms of a macrolide, and uses therefor Download PDF

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Publication number
HRP20160168T1
HRP20160168T1 HRP20160168T HRP20160168T HRP20160168T1 HR P20160168 T1 HRP20160168 T1 HR P20160168T1 HR P20160168 T HRP20160168 T HR P20160168T HR P20160168 T HRP20160168 T HR P20160168T HR P20160168 T1 HRP20160168 T1 HR P20160168T1
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Croatia
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cem
solution
water
peaks
radiation
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HRP20160168T
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Croatian (hr)
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David E Pereira
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Cempra Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/04—Nitro compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Claims (18)

1. Spoj CEM-101 formule [image] kristalne Forme I koji ima rendgenski difraktogram praškastog uzorka uključujući pikove na oko 2θ = 8.8, 10.5, 13.2, i 18.6; ili Forme II koji ima rendgenski difraktogram praškastog uzorka uključujući pikove na oko 2θ = 5.6, 7.9, 9.3, 11.7, 12.9, i 16.7; gdje je svaki od navedenih pikova detektiran od upadnog snopa Cu Kα zračenja, i je 60.2 2θ.1. Compound CEM-101 formula [image] crystalline Form I having an X-ray powder pattern including peaks at about 2θ = 8.8, 10.5, 13.2, and 18.6; or Form II having an X-ray powder pattern including peaks at about 2θ = 5.6, 7.9, 9.3, 11.7, 12.9, and 16.7; where each of the mentioned peaks was detected from the incident beam of Cu Kα radiation, and is 60.2 2θ. 2. Forma prema zahtjevu 1, naznačena time da uključuje Formu I, ili je Forma I CEM-101 koja ima rendgenski difraktogram praškastog uzorka s pikovima na 2θ = 8.8, 10.5, 13.2 i 18.6, koja je poželjno slobodna od Forme II CEM-101, još poželjnije, gdje su jedan ili više pikova na 2θ = 5.6, 9.8, i/ili 11.7 odsutni, gdje je svaki od navedenih pikova detektiran od upadnog snopa Cu Kα zračenja, i je 60.2 2θ.2. The form according to claim 1, characterized in that it includes Form I, or Form I is CEM-101 having an X-ray powder pattern with peaks at 2θ = 8.8, 10.5, 13.2 and 18.6, which is preferably free from Form II CEM-101 , more preferably, where one or more peaks at 2θ = 5.6, 9.8, and/or 11.7 are absent, where each of said peaks is detected from an incident beam of Cu Kα radiation, and is 60.2 2θ. 3. Forma prema zahtjevu 1, naznačena time da uključuje Formu II, ili je Forma II CEM-101 koja ima rendgenski difraktogram praškastog uzorka s pikovima na 2θ = 5.6, 7.9, 9.3, 11.7, 12.9 i 16.7, koja je poželjno slobodna od Forme I CEM-101, poželjnije, gdje su jedan ili više pikova na 2θ = 6.2 i/ili 8.8 odsutni, gdje je svaki od navedenih pikova detektiran od upadnog snopa Cu Kα zračenja, i je 60.2 2θ.3. Form according to claim 1, characterized in that it includes Form II, or Form II is CEM-101 having an X-ray powder pattern with peaks at 2θ = 5.6, 7.9, 9.3, 11.7, 12.9 and 16.7, which is preferably free from Form And CEM-101, more preferably, where one or more peaks at 2θ = 6.2 and/or 8.8 are absent, where each of said peaks is detected from an incident beam of Cu Kα radiation, and is 60.2 2θ. 4. Forma prema zahtjevu 1, naznačena time da je čista Forma I CEM-101.4. The form according to claim 1, characterized in that it is pure Form I CEM-101. 5. Forma prema zahtjevu 1, naznačena time da je čista Forma II CEM-101.5. The form according to claim 1, characterized in that it is pure Form II CEM-101. 6. Forma prema zahtjevu 1, naznačena time da je Forma I CEM-101 koja ima rendgenski difraktogram praškastog uzorka detektiran od upadnog snopa Cu Kα zračenja isti kao na SL. 1.6. Form according to claim 1, characterized in that Form I CEM-101 having the X-ray diffractogram of the powder sample detected from the incident beam of Cu Kα radiation is the same as in FIG. 1. 7. Forma prema zahtjevu 1, naznačena time da je Forma II CEM-101 koja ima rendgenski difraktogram praškastog uzorka detektiran od upadnog snopa Cu Kα zračenja isti kao na SL. 2.7. Form according to claim 1, characterized in that Form II CEM-101 having the X-ray diffractogram of the powder sample detected by the incident beam of Cu Kα radiation is the same as in FIG. 2. 8. Farmaceutski pripravak koji sadrži CEM-101 kristalne forme kao što je opisano u bilo kojem od zahtjeva 1-7 i nadalje sadrži najmanje jedan farmaceustki prihvatljiv nosač ili pomoćno sredstvo.8. A pharmaceutical composition comprising CEM-101 in crystalline form as described in any one of claims 1-7 and further comprising at least one pharmaceutically acceptable carrier or excipient. 9. Farmaceutski pripravak koji sadrži CEM-101 kristalne forme kao što je opisano u bilo kojem od zahtjeva 1-7 za uporabu u tretiranju bakterijske infekcije, protozoalne infekcije, ili poremećaja povezanog s bakterijskom infekcijom ili protozoalnom infekcijom.9. A pharmaceutical composition comprising CEM-101 in crystalline form as described in any one of claims 1-7 for use in treating a bacterial infection, a protozoal infection, or a disorder associated with a bacterial infection or a protozoal infection. 10. Uporaba CEM-101 kristalne forme kao što je opisano u bilo kojem od zahtjeva 1-7 ili farmaceutskog pripravka prema zahtjevu 8 za proizvodnju lijeka za tretiranje bakterijske infekcije, protozoalne infekcije, ili poremećaja povezanog s bakterijskom infekcijom ili protozoalnom infekcijom.10. Use of a CEM-101 crystalline form as described in any of claims 1-7 or a pharmaceutical composition according to claim 8 for the manufacture of a medicament for treating a bacterial infection, a protozoal infection, or a disorder associated with a bacterial infection or a protozoal infection. 11. Uporaba prema bilo kojem od zahtjeva 9 i 10, naznačeno time da je subjekt sisavac, riba, ptica ili reptil, poželjno čovjek.11. Use according to any one of claims 9 and 10, characterized in that the subject is a mammal, fish, bird or reptile, preferably a human. 12. Postupak za dobivanje Forme I CEM-101 prema zahtjevu 1, naznačeno time da postupak obuhvaća korak dodavanja otopine CEM-101 u s vodom miješljivim, polarnim organskim otapalom u vodu pri temperaturi ispod 50 C, poželjno pri čemu je forma I CEM-101 slobodna od drugih fizičkih formi.12. Process for obtaining Form I CEM-101 according to claim 1, characterized in that the process comprises the step of adding a solution of CEM-101 in a water-miscible, polar organic solvent to water at a temperature below 50 C, preferably in which Form I CEM-101 is free from other physical forms. 13. Proces prema zahtjevu 12 nadalje sadrži jedan ili više slijedećih koraka: zagrijavanje otopine CEM-101; filtriranje otopine CEM-101; reduciranje volumena otopine CEM-101 evaporacijom; i miješanje vode tijekom dodavanja otopine CEM-101.13. The process according to claim 12 further contains one or more of the following steps: heating the CEM-101 solution; filtering the CEM-101 solution; reducing the volume of the CEM-101 solution by evaporation; and mixing the water while adding the CEM-101 solution. 14. Proces prema zahtjevu 13, naznačen time da je otapalo aceton, metanol ili etanol, ili njihova kombinacija, najpoželjnije gdje je otapalo aceton.14. The process according to claim 13, characterized in that the solvent is acetone, methanol or ethanol, or their combination, most preferably where the solvent is acetone. 15. Proces prema zahtjevu 14, naznačen time da se otopina dodaje u vodu pri temperaturi od 10 C do 30 C.15. Process according to claim 14, characterized in that the solution is added to water at a temperature of 10 C to 30 C. 16. Proces za pripravu Forme II CEM-101 prema zahtjevu 1, poželjno slobodne od drugih fizičkih formi, naznačeno time da proces sadrži korak dodavanja vode otopini CEM-101 u s vodom miješljivim, polarnim organskim otapalom.16. Process for the preparation of Form II CEM-101 according to claim 1, preferably free from other physical forms, characterized in that the process contains the step of adding water to a solution of CEM-101 in a water-miscible, polar organic solvent. 17. Proces prema zahtjevu 16 nadalje sadrži jedan ili više od slijedećih koraka: filtriranje otopine CEM-101; reduciranje volumena otopine CEM-101 evaporacijom; i miješanje otopine CEM-101 tijekom dodavanja vode, poželjno gdje je otapalo aceton, acetonitril, 1,4-dioksan, metanol ili etanol, ili njihova kombinacija, poželjnije gdje je otopina CEM-101 na temperaturi iznad ambijentalne.17. The process according to claim 16 further comprises one or more of the following steps: filtering the CEM-101 solution; reducing the volume of the CEM-101 solution by evaporation; and stirring the CEM-101 solution while adding water, preferably where the solvent is acetone, acetonitrile, 1,4-dioxane, methanol or ethanol, or a combination thereof, more preferably where the CEM-101 solution is at above ambient temperature. 18. Postupak za pročišćavanje CEM-101 koji obuhvaća pretvaranje jedne ili više formi ili mješavina formi CEM-101 u Formu I ili Formu II, svaki prema zahtjevu 1, postupak obuhvaća korak dodavanja otopine CEM-101 u s vodom miješljivim, polarnim organskim otapalom u vodu pri temperaturi ispod 50 C; ili postupak sadrži korak dodavanja vode u otopinu CEM-101 u s vodom miješljivim, polarnim organskim otapalom.18. A process for purifying CEM-101 comprising converting one or more forms or mixtures of forms of CEM-101 to Form I or Form II, each according to claim 1, the process comprising the step of adding a solution of CEM-101 in a water-miscible, polar organic solvent to water at a temperature below 50 C; or the process comprises the step of adding water to a solution of CEM-101 in a water-miscible, polar organic solvent.
HRP20160168T 2010-03-22 2016-02-16 Crystalline forms of a macrolide, and uses therefor HRP20160168T1 (en)

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Application Number Priority Date Filing Date Title
US31606310P 2010-03-22 2010-03-22
EP11760068.4A EP2550286B1 (en) 2010-03-22 2011-03-22 Crystalline forms of a macrolide, and uses therefor
PCT/US2011/029424 WO2011119604A1 (en) 2010-03-22 2011-03-22 Crystalline forms of a macrolide, and uses therefor

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JP (4) JP5711352B2 (en)
KR (2) KR102006200B1 (en)
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